NOVEL INTERMEDIATE AND PROCESSES FOR ITS PREPARATION AND CONVERSION INTO A PHARMACOLOGICALLY-ACTIVE AGENT

摘要

Processes for the preparation of Venlafaxine (IX) via the novel epoxy- nitrile intermediate (I), which when subjected to hydrogenation forms compound (X), and may subsequently be reduced to yield the desired product (IX). The epoxy-nitrile intermediate (I) itself may be synthesised via vario us alternative reaction strategies, from a range of starting materials. E.g. 4- methoxy-benzaldehyde (VI), upon treatment with cyclohexyl magnesium bromide yields compound (V). This in turn may be oxidised to yield compound (III), which forms compound (II) on treatment with an .alpha.-keto- halogenation agent. Cyanation of compound (II), then yields the desired epoxy nitrile intermediate (I), from which Venlafaxine (IX) may be synthesised.